A5025879593- Peptidase Inhibition and Analysis
- Biochemical and Molecular Research
- Malaria Research and Control
- Endoplasmic Reticulum Stress and Disease
- Computational Drug Discovery Methods
- Tuberculosis Research and Epidemiology
- Synthesis and biological activity
- HIV/AIDS drug development and treatment
- Synthesis and Biological Evaluation
- Ubiquitin and proteasome pathways
- Synthesis and Characterization of Heterocyclic Compounds
- X-ray Diffraction in Crystallography
- Enzyme function and inhibition
- Research on Leishmaniasis Studies
- Antibiotic Resistance in Bacteria
- Mycotoxins in Agriculture and Food
- Molecular Sensors and Ion Detection
- Mycobacterium research and diagnosis
- Quinazolinone synthesis and applications
- Crystallization and Solubility Studies
- Porphyrin and Phthalocyanine Chemistry
- Click Chemistry and Applications
- Luminescence and Fluorescent Materials
- Adenosine and Purinergic Signaling
- Fungal Plant Pathogen Control
University of Delhi
2011-2020
University of Saskatchewan
2017
Magna Graecia University
2010
University College of Medical Sciences
2010
Indian Veterinary Research Institute
2010
Sapienza University of Rome
2010
American College of Chest Physicians
2010
Centre of Biomedical Research
2008
Novozymes (Denmark)
2008
A novel transacetylase (TAase) function of glutamine synthetase (GS) in bacterial species such as Mycobacterium smegmatis and tuberculosis H37Rv was established by us, termed mycobacterial TAase (MTAase). Several polyphenolic acetates (PAs) were found to be substrates for MTAase inhibiting certain receptor proteins glutathione S-transferase way acetylation. The present work describes the descriptor-based 2D-QSAR studies developed a series PA synthesized us evaluated antimycobacterial...
The objective of the present study was to evaluate antitubercular activity amino and acyl derivatives coumarins when used alone in combination with isoniazid, rifampicin, streptomycin or ethambutol, decipher mode action most effective agent. A series were synthesized screened for against Mycobacterium tuberculosis H37Rv strain. These compounds further evaluated by standard assay procedures determine their MBCs, fractional inhibitory concentration index values cytotoxicities. MICs a...
A series of novel triazine–pyrimidine hybrids have been synthesized and evaluated for their<italic>in vitro</italic>antimalarial activity.
Peroxisome proliferator-activated receptor gamma (PPAR γ ) is a potential target for the treatment of several disorders. In view FDA approved kinase inhibitors, in current study, we have investigated interaction selected inhibitors with PPAR using computational modeling, docking, and molecular dynamics simulations (MDS). The docked conformations MDS studies suggest that KIs interact ligand binding domain (LBD) high positive predictive values. Hence, first time shown plausible site. results...
To evade the possible toxicity associated with formation of quinone-imine metabolite in amodiaquine (AQ), para-hydroxyl group was replaced a -F atom, and resulting 4'-fluoro-amodiaquine (FAQ) hybridized substituted pyrimidines. The synthesized FAQ-pyrimidines displayed better vitro potency than chloroquine (CQ) against resistant P. falciparum strain (Dd2), exhibiting up to 47.3-fold activity (IC50: 4.69 nM) CQ 222 2.8-fold artesunate 13.0 nM). Twelve compounds exhibited antiplasmodial...
A series of novel 4-aminoquinoline–pyrimidine hybrids was synthesized and evaluated for their antimalarial activity.
Novel 4-aminoquinoline–pyrimidine based antimalarial hybrids were discovered to show potent activity against NF54 and Dd2 strains of<italic>P. falciparum.</italic>
4-Aminoquinoline-pyrimidine-aminoalkanols displaying good<italic>in vitro</italic>antimalarial activities against both CQ-sensitive and -resistant strains of<italic>P. falciparum</italic>, together with favourable resistance-indices the predicted ADME properties, are reported.
Journal Article Protein acyltransferase function of purified calreticulin. Part 1: characterization propionylation protein utilizing propoxycoumarin as the propionyl group donor Get access Prabhjot Singh, Singh 1Department Biochemistry, V.P. Chest Institute; 2Department Chemistry, University Delhi, Delhi 110007, India; 3Dipartimento di Medicina Sperimentale e Clinica, Università Catanzaro 'Magna Græcia' Campus 'S. Venuta', Loc. Germaneto 88100, Catanzaro, Italy; 4Division Indian Veterinary...
Earlier observations carried out in our laboratory highlighted the mode of action acetoxy 4-meth-ylcoumarins and quercetin pentaacetate preventing genotoxicity aflatoxin B1 (AFB1). We have extended observation to an biscoumarin i.e. ellagic acid peracetate (EAPA), which unlike (EA) has demonstrated time-dependent inhibition liver microsomes catalysed AFB1-epoxidation as measured by AFB1 binding DNA. EAPA was more potent than EA bone marrow lung cells from AFB1-induced genotoxicity. acted...
Abstract Background The presence of four mammalian cell entry ( mce ) operons in Mycobacterium tuberculosis suggests the essentiality functions genes these operons. differential expression different phases vitro growth and infected animals reported earlier from our laboratory further justifies apparent redundancy for genome. Here we investigate extent polymorphism eight mce1 mce4 M. standard reference strains (H37Rv, H37Ra, LVS (Low Virulent Strain) BCG) 112 clinical isolates varying their...
The distinct biochemical function of endoplasmic reticulum (ER) protein Calreticulin (CR) catalyzing the transfer acyl group from acyloxycoumarin to a receptor was termed calreticulin transacylase (CRTAase). present study, unlike previous reports others utilizing CR-deficient cells alone, dealt with recombinant CR domains Heamonchus contortus (rhCRTAase) in order examine their CRTAase activity. P-domain rhCR N- and C-domains found be endowed function. We have also observed for first time...
A series of antimalarial 4-aminoquinoline-pyrimidine hybrids incorporating modified anilines at the pyrimidine end was designed and synthesized through a facile synthetic route. The present displayed excellent equipotent in vitro antiplasmodial activities against both chloroquine-sensitive (D6) chloroquine-resistant (W2) strains P. falciparum with up to 11-fold (IC50=0.033 μM) better activity than reference drug, (chloroquine, IC50=0.370 resistant strain. compounds were found be...
Abstract Earlier reports from our laboratory established the acetyl transferase function of calreticulin (CRT), enabling CRT to transfer groups acetoxy polyphenolic acetates (PAs) certain receptor proteins. We have in this paper documented ability catalyze possible moiety 7-acetamido-4-methylcoumarin (7-N-AMC) proteins, glutathione S-transferase (GST), and NADPH cytochrome c reductase, leading modification their catalytic activities. 7-Acetoxy-4-methylthiocoumarin (7-AMTC) compared...